• Title/Summary/Keyword: Fragment size

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HQSAR Study of Microsomal Prostaglandin E2 Synthase (mPGES-1) Inhibitors

  • San Juan, Amor A.;Cho, Seung-Joo;Cho, Hoon
    • Bulletin of the Korean Chemical Society
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    • v.27 no.10
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    • pp.1531-1536
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    • 2006
  • Microsomal prostaglandin $E_2$ synthase (mPGES-1) is an enzyme that is associated with inflammation, pain, fever and cancer. Hologram quantitative structure activity relationship (HQSAR) was conducted on the series of MK-886 compounds acting as mPGES-1 inhibitors. A training set with 24 compounds was used to establish the HQSAR model. The best model was chosen based on the cross-validated correlation coefficient ($q^2$=0.884) and the correlation coefficient($r^2$=0.976). The model was utilized to predict the activity of the eight-test set of compounds giving the predictive $r^2$ value of 0.845. The descriptors of the model are based on fragment distinction (atoms, bond and connectivity) and fragment size (2-5 atoms). The atomic contribution maps generated from HQSAR were useful in identifying the important structural features responsible for the inhibitory activity of MK-886 inhibitors. Based on the generated model, the presence of hydrophobic biphenyl group seems to enhance inhibition of mPGES-1 that is in agreement with the previous experiments. In addition, it seems important for a halogen to be substituted to the biphenyl ring and for an acyl group to be attached to the indole moiety for enhanced activity.

Cloning and Expression of Leu 2 Gene (${\beta}-isopropylmalate$ dehydrogenase) from the Basidiomycete Flammulina velutipes in E. coli (팽나무버섯 균사체에서 ${\beta}-isopropylmalate$ dehydrogenase(Leu 2) gene 의 cloning 및 E. coli에서 발현)

  • Byun, Myung-Ok;Yoo, Young-Bok;Go, Seung-Joo;You, Chang-Hyun;Cha, Dong-Yul;Park, Yong-Hwan
    • The Korean Journal of Mycology
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    • v.17 no.1
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    • pp.35-38
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    • 1989
  • Gene libraries of DNA from Flammulina velutipes were constructed using Escherichia coli plasmid pBR 322. Leu 2 gene coding ${\beta}-isopropylmalate$ dehydrogenase from F. velutipes was cloned by complementation of leucine requiring mutant of E. coli. The size of inserted DNA fragment of this clone is about 1 Kbp. The fragment has Bam H1 and Ava 1 restriction sites.

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Hologram Based QSAR Analysis of Caspase-3 Inhibitors

  • Sathya., B
    • Journal of Integrative Natural Science
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    • v.11 no.2
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    • pp.93-100
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    • 2018
  • Caspases, a family of cysteinyl aspartate-specific proteases plays a central role in the regulation and the execution of apoptotic cell death. Caspase-3 has been proven to be an effective target for reducing the amount of cellular and tissue damage because the activation of caspases-3 stimulates a signalling pathway that ultimately leads to the death of the cell. In this study, Hologram based Quantitative Structure Activity Relationship (HQSAR) models was generated on a series of Caspase-3 inhibitors named 3, 4-dihydropyrimidoindolones derivatives. The best HQSAR model was obtained using atoms, bonds, and hydrogen atoms (A/B/H) as fragment distinction parameter using hologram length 61 and 3 components with fragment size of minimum 5 and maximum 8. Significant cross-validated correlation coefficient ($q^2=0.684$) and non cross-validated correlation coefficients ($r^2=0.754$) were obtained. The model was then used to evaluate the eight external test compounds and its $r^2_{pred}$ was found to be 0.559. Contribution map show that presence of pyrrolidine sulfonamide ring and its bulkier substituent's makes big contributions for improving the biological activities of the compounds.

Orbital wall restoring surgery with primary orbital wall fragments in blowout fracture

  • Kang, Dong Hee
    • Archives of Craniofacial Surgery
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    • v.20 no.6
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    • pp.347-353
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    • 2019
  • Most orbital surgeons believe that it's difficult to restore the primary orbital wall to its previous position and that the orbital wall is so thin that cannot be firmly its primary position. Therefore, orbital wall fractures generally have been reconstructed by replacing the bony defect with a synthetic implant. Although synthetic implants have sufficient strength to maintain their shape and position in the orbital cavity, replacement surgery has some drawbacks due to the residual permanent implants. In previous studies, the author has reported an orbital wall restoring technique in which the primary orbital wall fragment was restored to its prior position through a combination of the transorbital and transantral approaches. Simple straight and curved elevators were introduced transnasally to restore the orbital wall and to maintain temporary extraorbital support in the maxillary and ethmoid sinus. A transconjunctival approach provided sufficient space for implant insertion, while the transnasal approach enabled restoration of the herniated soft tissue back into the orbit. Fracture defect was reduced by restoring the primary orbital wall fragment to its primary position, making it possible to use relatively small size implant, furthermore, extraorbital support from both sinuses decreased the incidence of implant displacement. The author could recreate a natural shape of the orbit with the patient's own orbital bone fragments with this dual approach and effectively restored the orbital volume and shape. This procedure has the advantages for retrieving the orbital contents and restoring the primary orbital wall to its prior position.

Cloning of Pectate Lyase Gene of Alkali-tolerant Bacillus sp. YA-14 and Its Expression in Escherichia coli (알카리 내성 Bacillus sp. YA-14의 Pectate Lyase 유전자의 클로닝과 발현)

  • Yu, Ju-Hyun;Park, Yoon-Suk;Kim, Jin-Man;Kong, In-Soo;Chung, Yong-Joon
    • Microbiology and Biotechnology Letters
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    • v.16 no.4
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    • pp.316-319
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    • 1988
  • Pectate Lyase (PL) was cloned from alkali-tolerant Bacillus sp. YA-14 into Escherichia coli MB1000 by inserting HindIII-generated DNA fragment into the HindIII site of pBR322 and then screening recombinant transformant for the ability to hydrolyze sodium polypectate on agar plate, The recombinant plasmid, called pYPC29, was isolated, and the size of the cloned HindIII fragment was found to be 1.6 kb. The PL gene was stablely maintained and expressed efficiently in Escherichia coli. The Pt accumulated largely in the periplasmic space of Escherichia coli clones.

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Synthesis of Cyclic Peticdes Related to GBⅠ-Ⅱand Study of Their Inhibitory Activity for Proteinases (GBⅠ-Ⅱ 와 관련된 Cyclic Peptide 들의 합성과 단백질 분해 효소에 대한 저해활성 연구)

  • Gang, Sin Won;Heo, Nam Won
    • Journal of the Korean Chemical Society
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    • v.34 no.3
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    • pp.288-296
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    • 1990
  • Antielastic fragment in GBⅠ-Ⅱ differ on $P_1$ site with that of antitryptic fragment in LBI. To obtain further understanding of the role of amino acid residue near the reactive site, specificity of $P_1$ site and loop size, Tyr substituted cyclic nonapeptide and cyclic pentapeptide were synthesized and the inhibition constants for some proteinases were calculated by Dixon method. Cyclic nonapeptide showed no inhibition for chymotrypsin but appeared low inhibitory activity for trypsin and elastase and that of cyclic pentapeptide possessed inhibitory activity for chymotrypsin.

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Genetic Studies on Korean Anurans: Length and Restriction Site Variation in the Mitochondrial DNA of Tree Frogs, Hyla japonica and H. suweonensis (한국산 무미류에 대한 유전학적 연구 : 청개구리속 2종(Hyla japonira, H. suweonensis)에 대한 mtDNA의 크기 및 제한효소 인식위치의 변이)

  • 이혜영;박창신
    • The Korean Journal of Zoology
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    • v.35 no.2
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    • pp.219-225
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    • 1992
  • The genetic variation in mitochondrial DNA (mtDNA) was analysed within and between two species of tree frogs. Hyla japonica and H. suweonensis from South Korea. Purified mtDNAs were digested with each of 11 restriction enLvmes which cleave at six base recognition sequences. The genome size of H. iaponica revealed ho types (20.0 $\pm$ 0.3 and 19.6 $\pm$ 0.3 kb) and this difference is explained by either addition or deletion of about 0.4 kb fragment. On the other hand, the genome sire of H. suueonensis was about 19.0 $\pm$ 0.4 kb only. For the analysis, level of fragment homology (F) and nucleotide sequence divergence (p) were estimated from comparisons of digestion profiles. Among four populations of H. iaponica, substantial mean sequence divergence was 0.017 (range 0.001-0.026); between identical types, 0.001 IslilaRl type) and 0.004 (Large type) respectively; between different ones, 0.024 (range 0.023-0.026). The level of sequence divergence between he species was 0.142 (range 0.131-0.146). This result suggested that he species ㅂwere distinctly differentiated species. The divergence time between ko species was estimated 7.1 million years.

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Asynchronous and Adaptive Massage Passing Scheme for Wireless Sensor Networks (무선 센서 네트워크를 위한 비동기 적응형 메시지 전달 기법)

  • Jeong, Jong-Kyun;Ra, In-Ho
    • Journal of the Korean Institute of Intelligent Systems
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    • v.23 no.3
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    • pp.196-201
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    • 2013
  • In this paper, we propose an asynchronous and adaptive message passing scheme based on S-MAC for handling with the problem on energy efficiency in wireless sensor networks. The proposed scheme consists of a policy that differentiate transmission errors caused by packet collision or radio interference from congestion errors caused by buffer overflow and a method that adaptively controls the size of a fragment according to the variance of traffic loads. Especially, it presents a method that highly reduce the energy consumption by keeping the size of fragment not being excessively smaller than the one that may result in rapid increment of the total transfer time. Finally, with the simulation results we show that network throughput and delay are improved by using the proposed message passing scheme.

Blast Design for Explosive Demolition of Concrete Foundation (기초콘크리트 구조물의 발파해체를 위한 발파설계)

  • Park, Hoon;Park, Hyoung-Ki;Suk, Chul-Gi;Yi, Young-Seop;Kaneko, Katsuhiko
    • Explosives and Blasting
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    • v.30 no.1
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    • pp.9-16
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    • 2012
  • With the deterioration and functional loss of structures, there is an increasing demand for demolition and various demolition technologies have been developed. In case of a large-scale concrete foundation, application of some mechanical demolition techniques is limited because of the structural characteristics, and explosive demolition or explosive demolition combined with mechanical demolition is applied recently due to the effect to the surrounding environment by the ground vibration. In this study, we compared peak particle velocity of ground vibration depending on average fragment size in case of explosive demolition design for large-scale concrete foundation using the relation among specific charge, charge constant and transmitting medium constant as well as the relation between average concrete fragment size and specific charge.

Energy Efficient Transmission Parameters Analysis of TDMA Based HR-WPAN System for Ship Environment (선박환경에서 에너지 효율성을 고려한 TDMA기반 고속 WPAN시스템의 전송파라미터 분석)

  • Park, Young-Min;Lee, Woo-Young;Lee, Seong-Ro;Lee, Yeon-Woo
    • The Journal of Korean Institute of Communications and Information Sciences
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    • v.34 no.9A
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    • pp.712-718
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    • 2009
  • This paper proposes the optimal transmission parameter selection method for an energy efficient Wireless Personal Area Network (WPAN) system which is applicable to the Maritime Telematics targeting for various ship models. Since the transmission parameter selection is an important factor for WPAN system to decide its energy efficiency, we propose an energy consumption model for ship area network (SAN) employing IEEE 802.15.3 based TDMA HR-WPAN model and analyzes the effect of transmission parameter selection on the performance of energy consumption. In particular, the main performance decision parameter of the SAN applying HR-WPAN is path loss, since it is very varied according to the material of shipbuilding such as steel (large ship), FRP (medium size ship) and compound wood (small ship). Thus, we analyzed and demonstrated that the proper transmission parameter selection among transmit power, PHY data rate and fragment size for each ship model guarantee the energy efficiency.